49787-00-0Relevant articles and documents
Synergism of a novel 1,2,4-oxadiazole-containing derivative with oxacillin against methicillin-resistant staphylococcus aureus
Buommino, Elisabetta,D’auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Piccolo, Marialuisa,Sciarretta, Martina
, (2021/11/01)
Staphylococcus aureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in
VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 0236, (2020/01/24)
Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
SSAO INHIBITOR
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Paragraph 0234-0236; 0277-0279, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
FUNGICIDAL OXADIAZOLES
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Paragraph 0673, (2020/06/07)
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
NOVEL OXADIAZOLE DERIVATIVE AND PHARMACEUTICAL CONTAINING SAME
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Paragraph 0136; 0137, (2018/02/28)
An amyloid fibril formation inhibitor comprising a compound represented by the following general formulae (I) to (III): wherein Q is -C(=O)-; X is -C(=O)-, -NH-C(=O)-; Y is -(CH2)m-; Z is -(CH2)n-; R1
Synthesis of novel mono and bis nitric oxide donors with high cytocompatibility and release activity
Sahyoun, Tanya,Gaucher, Caroline,Zhou, Yi,Ouaini, Na?m,Schneider, Rapha?l,Arrault, Axelle
supporting information, p. 3329 - 3332 (2018/09/27)
Four compounds bearing amidoxime functions were synthetized: (1) 2a,b bearing an aromatic amidoxime function, (2) 2c bearing an aliphatic amidoxime function, and (3) 2d bearing aromatic and aliphatic amidoximes functions. The ability of these compounds to
Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan
Naro, Yuta,Ankenbruck, Nicholas,Thomas, Meryl,Tivon, Yaniv,Connelly, Colleen M.,Gardner, Laura,Deiters, Alexander
, p. 5900 - 5909 (2018/08/04)
Chemical probes of microRNA (miRNA) function are potential tools for understanding miRNA biology that also provide new approaches for discovering therapeutics for miRNA-associated diseases. MicroRNA-21 (miR-21) is an oncogenic miRNA that is overexpressed in most cancers and has been strongly associated with driving chemoresistance in cancers such as renal cell carcinoma (RCC). Using a cell-based luciferase reporter assay to screen small molecules, we identified a novel inhibitor of miR-21 function. Following structure-activity relationship studies, an optimized lead compound demonstrated cytotoxicity in several cancer cell lines. In a chemoresistant-RCC cell line, inhibition of miR-21 via small molecule treatment rescued the expression of tumor-suppressor proteins and sensitized cells to topotecan-induced apoptosis. This resulted in a >10-fold improvement in topotecan activity in cell viability and clonogenic assays. Overall, this work reports a novel small molecule inhibitor for perturbing miR-21 function and demonstrates an approach to enhancing the potency of chemotherapeutics specifically for cancers derived from oncomir addiction.
ANTI-ENTEROVIRUS 71 THIADIAZOLIDINE DERIVATIVE
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Paragraph 0153-0155, (2017/03/28)
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
1, 2, 4-oxdiazole compound and its preparation method and application
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Paragraph 0066-0069, (2016/10/07)
The invention discloses a 1,2,4-oxadiazole compound and a preparation method and application thereof. The structural general formula of the compound is shown in a formula I. The preparation method comprises the following steps of: when RB is -CF3, perform
Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents
dos Santos Filho, José Maurício,de Queiroz e Silva, Diogo Manoel Alves,Macedo, Taís Soares,Teixeira, Helena Mariana Pitangueira,Moreira, Diogo Rodrigo Magalhaes,Challal, Soura,Wolfender, Jean-Luc,Queiroz, Emerson Ferreira,Soares, Milena Botelho Pereira
, p. 5693 - 5701 (2016/11/09)
Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, sy